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Related Concept Videos

Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
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G-protein Coupled Receptors01:21

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G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors01:21

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G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
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Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
Transducer Mechanism: G Protein–Coupled Receptors01:30

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
G Protein-coupled Receptors01:15

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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HSV-Mediated Transgene Expression of Chimeric Constructs to Study Behavioral Function of GPCR Heteromers in Mice
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5-HT(3) receptors.

Sarah C R Lummis1

  • 1Department of Biochemistry, University of Cambridge, Cambridge CB2 1QW, UK. sl120@cam.ac.uk

The Journal of Biological Chemistry
|October 6, 2012
PubMed
Summary
This summary is machine-generated.

5-Hydroxytryptamine type 3 (5-HT3) receptors are crucial in the nervous system. Understanding their structure aids in developing anti-nausea drugs like setrons.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • 5-Hydroxytryptamine type 3 (5-HT3) receptors are cation-selective Cys-loop receptors present in the central and peripheral nervous systems.
  • Five receptor subunits (A-E) exist, with the A subunit being essential for functional receptors.

Purpose of the Study:

  • To elucidate the structural basis of the agonist-binding site in 5-HT3 receptors.
  • To identify key amino acid residues involved in drug binding and receptor function.

Main Methods:

  • Analysis of receptor subunit sequences to identify regions contributing to the agonist-binding site.
  • Identification of specific amino acid residues within the binding pocket.

Main Results:

  • Noncontiguous regions of the receptor subunit sequence assemble to form the agonist-binding site.
  • The roles of various amino acid residues in the binding pocket have been characterized.

Conclusions:

  • Detailed knowledge of the 5-HT3 receptor binding site aids in understanding receptor pharmacology.
  • This information is critical for the development of novel therapeutics, particularly setrons, for nausea and vomiting.